Disposition and metabolic profiling of the penetration enhancer Azone. I. In vitro studies: Urinary profiles of hamster, rat, monkey, and man

Journal Article · Tue May 01 00:00:00 EDT 1990 · Pharmaceutical Research; (USA)

DOI:https://doi.org/10.1023/A:1015864632474· OSTI ID:6643094

Wiechers, J W; Drenth, B F; Adolfsen, F A; Prins, L; de Zeeuw, R A ^[1]

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1. Groningen Centre for Drug Research (Netherlands)

Chain-labeled {sup 14}C-Azone was intravenously administered to hamster, monkey, and rat, to compare its metabolic profile with that obtained previously in humans after dermal application. Azone-derived radioactivity was excreted predominantly in the urine for both hamster and monkey, which is similar to the disposition in humans. Metabolic profiling in urine revealed extensive systemic metabolism to occur in all species studied. The main fraction of the metabolites was most polar in man, followed by rat, monkey, and hamster. Traces of the parent compound were detectable only in hamster urine. Although some of the polar major human metabolites were also present in rat urine, the animals were unsuitable for collecting metabolites of Azone observed in humans. In rats, complete cleavage of the dodecyl side chain was ruled out by administering Azone that had been labeled at two distinct positions of the molecule. Additionally, oral administration of Azone to rats resulted in the same metabolic profile as intravenous administration, indicating that gastrointestinal metabolism does not occur or is similar to systemic metabolism.

• OSTI ID: 6643094
• Journal Information: Pharmaceutical Research; (USA), Vol. 7:5; ISSN 0724-8741
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
DRUGS
METABOLISM
CARBON 14 COMPOUNDS
FECES
HAMSTERS
INTRAVENOUS INJECTION
KIDNEYS
LIQUID COLUMN CHROMATOGRAPHY
MAN
MONKEYS
ORAL ADMINISTRATION
RATS
TRACER TECHNIQUES
ANIMALS
BIOLOGICAL MATERIALS
BIOLOGICAL WASTES
BODY
CHROMATOGRAPHY
INJECTION
INTAKE
ISOTOPE APPLICATIONS
LABELLED COMPOUNDS
MAMMALS
MATERIALS
ORGANS
PRIMATES
RODENTS
SEPARATION PROCESSES
VERTEBRATES
WASTES
550501* - Metabolism- Tracer Techniques